HUP0302862A2 - Tricyclic 2-pyridone compounds useful as hiv reverse transcriptase inhibitors, process for their preparation and pharmaceutical compositions containing them - Google Patents

Tricyclic 2-pyridone compounds useful as hiv reverse transcriptase inhibitors, process for their preparation and pharmaceutical compositions containing them

Info

Publication number
HUP0302862A2
HUP0302862A2 HU0302862A HUP0302862A HUP0302862A2 HU P0302862 A2 HUP0302862 A2 HU P0302862A2 HU 0302862 A HU0302862 A HU 0302862A HU P0302862 A HUP0302862 A HU P0302862A HU P0302862 A2 HUP0302862 A2 HU P0302862A2
Authority
HU
Hungary
Prior art keywords
general formula
group
carbonyl
nitrogen atom
reverse transcriptase
Prior art date
Application number
HU0302862A
Other languages
Hungarian (hu)
Inventor
Argyrios Arvanitis
Anthony J. Cocuzza
Mona Patel
James D. Rodgers
Haisheng Wang
Original Assignee
Bristol-Myers Squibb Pharma Co.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Bristol-Myers Squibb Pharma Co. filed Critical Bristol-Myers Squibb Pharma Co.
Publication of HUP0302862A2 publication Critical patent/HUP0302862A2/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • A61K31/7072Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Virology (AREA)
  • General Chemical & Material Sciences (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Engineering & Computer Science (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

A találmány tárgyát a HIV-reverz transzkriptáz inhibitoraikénthasználható általános képletű triciklusos piridonszármazékok - ahol Aegy általános képletű gyűrű; P jelentése oxigén- vagy kénatom; Wnitrogénatom vagy CR3 általános képletű csoport; X nitrogénatom vagyCR3a általános képletű csoport; Y nitrogénatom vagy CR3b általánosképletű csoport; Z nitrogénatom vagy CR3c általános képletű csoport;azzal a feltétellel, hogy ha W, X, Y és Z közül kettőnek a jelentésenitrogénatom, akkor a többi szubsztituens nitrogénatomtól eltérőjelentésű; R1 adott esetben halogénatommal szubsztituált alkilcsoport,ciklopropil-, hidroxi-metil- vagy cianocsoport; R2 adott esetbenszubsztituált alkil-, alkenil-, alkinil-, cikloalkil-, fenilcsoportvagy heterogyűrű; R8 hidrogénatom, alkil-karbonil-, alkoxi-, alkoxi-karbonil-, aril-oxi-, aril-oxi-karbonil-, aril-metil-karbonil-,(alkilkarbonil-oxi)-karbonil-, (aril-karbonil-oxi)-(alkoxi-karbonil)-,alkil-amino-karbonil-, fenil-amino-karbonil-, fenil-alkoxi-karbonil-vagy -NR5R5a-alkil-karbonilcsoport - ezeket tartalmazógyógyszerkészítmények és készletek, alkalmazásuk, valamint avegyületek előállítására szolgáló eljárások és azok közbenső termékeiképezik. ÓThe subject of the invention are tricyclic pyridone derivatives of the general formula that can be used as HIV reverse transcriptase inhibitors - where A is a ring of the general formula; P is oxygen or sulfur; A nitrogen atom or a group of general formula CR3; X is a nitrogen atom or a group with the general formula CR3a; Y is a nitrogen atom or a group of formula CR3b; Z is a nitrogen atom or a group of general formula CR3c; with the proviso that if two of W, X, Y and Z are nitrogen atoms, then the other substituents have different meanings from nitrogen atoms; R1 optionally substituted with a halogen atom, cyclopropyl, hydroxymethyl or cyano; R 2 is an optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, phenyl or hetero ring; R8 is hydrogen, alkylcarbonyl-, alkoxy-, alkoxycarbonyl-, aryloxy-, aryloxycarbonyl-, arylmethylcarbonyl-, (alkylcarbonyloxy)carbonyl-, (arylcarbonyloxy )-(Alkoxycarbonyl)-, alkyl-amino-carbonyl-, phenyl-amino-carbonyl-, phenyl-alkoxy-carbonyl- or -NR5R5a-alkylcarbonyl group - pharmaceutical preparations and kits containing these, their use, as well as the processes for the production of the compounds and their intermediate products. HE

HU0302862A 2000-07-20 2001-07-20 Tricyclic 2-pyridone compounds useful as hiv reverse transcriptase inhibitors, process for their preparation and pharmaceutical compositions containing them HUP0302862A2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US21953200P 2000-07-20 2000-07-20
US28485601P 2001-04-19 2001-04-19
PCT/US2001/022827 WO2002008226A2 (en) 2000-07-20 2001-07-20 Tricyclic 2-pyridone compounds useful as hiv reverse transcriptase inhibitors

Publications (1)

Publication Number Publication Date
HUP0302862A2 true HUP0302862A2 (en) 2003-12-29

Family

ID=26913986

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0302862A HUP0302862A2 (en) 2000-07-20 2001-07-20 Tricyclic 2-pyridone compounds useful as hiv reverse transcriptase inhibitors, process for their preparation and pharmaceutical compositions containing them

Country Status (23)

Country Link
US (1) US6596729B2 (en)
EP (1) EP1303515A2 (en)
JP (1) JP2004532793A (en)
KR (1) KR20030065454A (en)
CN (1) CN1464878A (en)
AR (1) AR031861A1 (en)
AU (1) AU2001280641A1 (en)
BG (1) BG107439A (en)
BR (1) BR0112606A (en)
CA (1) CA2418194A1 (en)
EE (1) EE200300027A (en)
HU (1) HUP0302862A2 (en)
IL (1) IL153683A0 (en)
IS (1) IS6690A (en)
LT (1) LT2003003A (en)
LV (1) LV13024B (en)
MX (1) MXPA03000434A (en)
NO (1) NO20030248L (en)
PL (1) PL365958A1 (en)
SI (1) SI21139A (en)
SK (1) SK392003A3 (en)
WO (1) WO2002008226A2 (en)
YU (1) YU3203A (en)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7638522B2 (en) 2001-08-13 2009-12-29 Janssen Pharmaceutica N.V. Salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino] benzonitrile
US8101629B2 (en) 2001-08-13 2012-01-24 Janssen Pharmaceutica N.V. Salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile
JO3429B1 (en) 2001-08-13 2019-10-20 Janssen Pharmaceutica Nv Hiv inhibiting pyrimidines derivatives
TW200306192A (en) 2002-01-18 2003-11-16 Bristol Myers Squibb Co Tricyclic 2-pyrimidone compounds useful as HIV reverse transcriptase inhibitors
AR039540A1 (en) * 2002-05-13 2005-02-23 Tibotec Pharm Ltd MICROBICIDE COMPOUNDS WITH PIRIMIDINE OR TRIAZINE CONTENT
JP4822707B2 (en) * 2002-08-09 2011-11-24 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ Process for producing 4-[[4-[[4- (2-cyanoethenyl) -2,6-dimethylphenyl] amino] -2-pyrimidinyl] amino] benzonitrile
US20070021449A1 (en) 2003-02-07 2007-01-25 Jan Heeres Pyrimidine derivatives for the prevention of hiv infection
TW200607503A (en) 2004-05-17 2006-03-01 Tibotec Pharm Ltd 1-heterocyclyl-1, 5-dihydro-pyrido[3, 2-b]indol-2-ones

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3700673A (en) * 1971-02-12 1972-10-24 Morton Norwich Products Inc 3-4-dihydrobenzo(b) (1,7)naphthyridin-1(2h)-ones
GB9023289D0 (en) 1990-10-25 1990-12-05 Ici Plc Herbicides
AU2436792A (en) * 1991-08-16 1993-03-16 Merck & Co., Inc. Quinazoline derivatives as inhibitors of hiv reverse transcriptase
IL102764A0 (en) 1991-08-16 1993-01-31 Merck & Co Inc Quinazoline derivatives,and pharmaceutical compositions containing them
DE4320347A1 (en) 1993-06-19 1994-12-22 Boehringer Mannheim Gmbh Quinazoline derivatives and medicaments containing them
AU1046895A (en) 1993-11-05 1995-05-23 Merck & Co., Inc. New quinazolines as inhibitors of hiv reverse transcriptase
DE4344452A1 (en) 1993-12-24 1995-06-29 Hoechst Ag Aza-4-iminoquinolines, process for their preparation and their use
ID18046A (en) 1996-08-20 1998-02-19 Takeda Chemical Industries Ltd COMPOUND, MIXED CYCLE, MANUFACTURE AND USE OF IT.
ATE248826T1 (en) 1996-10-02 2003-09-15 Bristol Myers Squibb Pharma Co 4,4-DISUBSTITUTED 1,4-DIHYDRO-2H-3,1-BENZOXAZINE-2-ONE APPLICABLE AS HIV REVERS TRANSCRIPTASE INHIBITORS, INTERMEDIATE PRODUCTS AND METHODS FOR THE PRODUCTION THEREOF
HRP980143A2 (en) 1997-04-09 1999-02-28 Soo Sung Ko 4,4-disubstituted-3,4-dihydro-2 (1h)-quinazolinones useful as hiv reverse transcriptase inhibitors
US6593337B1 (en) 1999-10-19 2003-07-15 Bristol-Myers Squibb Pharma Company Tricyclic compounds useful as HIV reverse transcriptase inhibitors

Also Published As

Publication number Publication date
MXPA03000434A (en) 2003-06-24
JP2004532793A (en) 2004-10-28
IL153683A0 (en) 2003-07-06
YU3203A (en) 2006-01-16
US6596729B2 (en) 2003-07-22
NO20030248L (en) 2003-03-17
IS6690A (en) 2003-01-17
AU2001280641A1 (en) 2002-02-05
PL365958A1 (en) 2005-01-24
BG107439A (en) 2003-09-30
WO2002008226A3 (en) 2002-06-20
KR20030065454A (en) 2003-08-06
US20020107261A1 (en) 2002-08-08
AR031861A1 (en) 2003-10-08
CN1464878A (en) 2003-12-31
SI21139A (en) 2003-08-31
WO2002008226A2 (en) 2002-01-31
CA2418194A1 (en) 2002-01-31
BR0112606A (en) 2004-06-29
EE200300027A (en) 2004-10-15
LV13024B (en) 2003-10-20
NO20030248D0 (en) 2003-01-17
EP1303515A2 (en) 2003-04-23
LT2003003A (en) 2003-11-25
SK392003A3 (en) 2003-10-07

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Legal Events

Date Code Title Description
FD9A Lapse of provisional protection due to non-payment of fees